A new method for the evaluation of benzodiazepines based on their ability to block muscimol-induced myoclonic jerks in mice.
A number of clinically used benzodiazepines were tested for their effectiveness in blocking muscimol-induced myoclonic jerks in mice. Their ED50 values were determined from their dose-response curves. These data gave the following relative potencies with respect to diazepam: diazepam = 1, medazepam = 0.24, oxazepam = 1.27, flurazepam = 1.90, lorazepam = 3.01, nitrazepam = 3.93, clonazepam = 33.14, and flunitrazepam = 116.00. Because our earlier studies indicated that muscimol-induced myoclonic jerks probably originate from the spinal cord, the present method may prove to be suitable for quantitatively evaluating the effect of benzodiazepines on the spinal cord. The present results also indicate the possible value of flunitrazepam in the management of neurologic disorders in which preferential action on the spinal cord is desired.
D000818:Animals; D001569:Benzodiazepines / Q000494:pharmacology*; D003975:Diazepam / Q000494:pharmacology; D004341:Drug Evaluation; D005445:Flunitrazepam / Q000494:pharmacology; D008297:Male; D051379:Mice; D009118:Muscimol / Q000037:antagonists & inhibitors*; D009207:Myoclonus / Q000139:chemically induced* / Q000517:prevention & control; D010080:Oxazoles / Q000037:antagonists & inhibitors*; D013116:Spinal Cord / Q000187:drug effects
D010080:Oxazoles; D001569:Benzodiazepines; D009118:Muscimol; D005445:Flunitrazepam; D003975:Diazepam